- |||||||||| Review, Journal, BRCA Biomarker, PARP Biomarker, IO biomarker: Synergistic strategies: ADC-PARP inhibitor combinations in triple-negative breast cancer therapy. (Pubmed Central) - Jul 20, 2025
Future directions include biomarker-driven patient selection, combination with immune checkpoint inhibitors, and advancement in next-generation ADCs. The synergistic potential of ADC-PARPi combinations provides a new avenue for overcoming TNBC resistance, enhancing treatment outcomes, and widening therapeutic strategies for this challenging disease.
- |||||||||| Xegafri (rociletinib) / Clovis
Journal: Covalent inhibition of ACSL4 alleviates ferroptosis-induced acute liver injury. (Pubmed Central) - Jul 19, 2025 Here, we identify Rociletinib (ROC) as a potent inhibitor of ferroptosis through virtual screening and mechanistic studies...ROC effectively mitigates ferroptosis-mediated acute liver injury in mouse models. These findings establish ROC as the targeted covalent inhibitor directly targeting ACSL4, offering a promising therapeutic strategy for ferroptosis-related diseases.
- |||||||||| Review, Journal, BRCA Biomarker, PARP Biomarker: Exploring the radiochemistry of PARP inhibitors: a new era in therapy and imaging. (Pubmed Central) - Jul 3, 2025
Finally, emerging evidence suggest the possibility to involve PARP-related radiopharmaceuticals in theranostics approaches. Despite challenges such as the complexity of radiolabelling, regulatory hurdles, and the need for more robust clinical validation, the continued exploration of the radiochemistry of PARP inhibitors promises to revolutionize both the diagnosis and treatment of cancer, offering hope for more effective and personalized cancer care.
- |||||||||| Journal, PARP Biomarker, PD(L)-1 Biomarker, IO biomarker: Update Gynecologic Malignancies 2025 - Expert Opinion on Systemic Therapy for Early and Advanced Gynecological Cancers. (Pubmed Central) - Jul 2, 2025
For ovarian cancer PARPi have shown substantial PFS benefits in key approval trials, including PRIMA for niraparib, PAOLA for olaparib, and ATHENA-MONO for rucaparib...Furthermore, mirvetuximab soravtansine is the first antibody-drug conjugate (ADC) approved in Germany for platinum-resistant ovarian cancer for patients with folate receptor alpha expression...With the increased use of ADCs, this is not the end of these developments. Therapy algorithms from a certified German oncology center are developed and presented in this article.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz, Lynparza (olaparib) / Merck (MSD), AstraZeneca
Review, Journal, BRCA Biomarker, PARP Biomarker: BRCA Mutation Testing in Men with Metastatic Castration-Resistant Prostate Cancer: Practical Guidance for Australian Clinical Practice. (Pubmed Central) - Jun 30, 2025 Here, we provide expert recommendations on how to optimize BRCA molecular diagnostic testing in patients with mCRPC. Optimization and standardization of molecular diagnostic testing will support health care providers and institutes in establishing more efficient testing pathways, enabling access to targeted therapies such as PARPi, and improving patient outcomes.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz, Lynparza (olaparib) / Merck (MSD), AstraZeneca
Engineering chromosomal instability via BRCA1/2 knockout in vitro (Poster and Exhibition Hall; Poster Board No EACR25-3216) - Jun 29, 2025 - Abstract #EACR2025EACR_827; These findings underscore the value of models harbouring isolated molecular defects in linking specific CIN patterns to their underlying causes and that our single-cell workflow accurately detects CIN-types in a premalignant scenario, which has not been possible to date given the limited resolution of standard bulk sequencing. Therefore, we are now increasing the collection of these models by knocking out 562 genes related to other DNA Damage Response pathways.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz, Lynparza (olaparib) / Merck (MSD), AstraZeneca, Zejula (niraparib) / GSK, J&J
Journal, Benefit-risk assessment, BRCA Biomarker, PARP Biomarker: Overall Survival and the Evolving Benefit-Risk Assessment for Poly (ADP-ribose) Polymerase Inhibitors in Advanced Ovarian Cancer. (Pubmed Central) - Jun 26, 2025 Recognizing the clinical implications of these regulatory actions, herein we describe the FDA's decision-making process and the rationale behind the removal or narrowing of these indications for PARP inhibitors in advanced EOC. Furthermore, this article provides insight into the FDA's interpretation of potential OS detriments and subgroup analyses to shape regulatory decisions.
- |||||||||| Opdivo (nivolumab) / Ono Pharma, BMS, Rubraca (rucaparib) / Pharma& Schweiz
Trial completion, Trial completion date, Trial primary completion date: A Study of Rucaparib and Nivolumab in People With Leiomyosarcoma (clinicaltrials.gov) - Jun 18, 2025 P2, N=20, Completed, Although there is a modest rise in the frequency of severe adverse reactions, they are usually handled well. Active, not recruiting --> Completed | Trial completion date: Nov 2025 --> Jun 2025 | Trial primary completion date: Nov 2025 --> Jun 2025
- |||||||||| Opdivo (nivolumab) / Ono Pharma, BMS, Rubraca (rucaparib) / Pharma& Schweiz
P2 data, Journal, BRCA Biomarker, PARP Biomarker, PD(L)-1 Biomarker, IO biomarker: Phase II study of rucaparib and nivolumab in patients with leiomyosarcoma. (Pubmed Central) - Jun 14, 2025 The addition of a PARP inhibitor did not improve the efficacy of ICI in LMS. Adverse events, especially due to overlapping toxicities, were frequent and often led to dose delays and modifications.
- |||||||||| AiRuiYi (fluzoparib) / Jiangsu Hengrui Pharma, Rubraca (rucaparib) / Pharma& Schweiz
Preclinical, Journal, BRCA Biomarker, PARP Biomarker: Bioanalytical assay for the quantification of rucaparib in rat plasma using UPLC-MS/MS: development, and validation for interaction with myricetin. (Pubmed Central) - Jun 10, 2025 The results of the drug-drug interaction (DDI) study showed that myricetin had no significant effect on the pharmacokinetic parameters of rucaparib, which indicating that the clinician did not need to adjust the dosage of rucaparib when it was used in combination. The UPLC-MS/MS method developed in this study was successfully used for the determination of the plasma concentrations of rucaparib orally administered in rats, which provided a reference for DDI studies and clinical pharmacokinetic studies of rucaparib.
- |||||||||| Review, Journal, BRCA Biomarker, PARP Biomarker, IO biomarker: PARP Inhibitors in Genitourinary Cancer: A New Paradigm Beyond Prostate Cancer. (Pubmed Central) - Jun 9, 2025
More recently, pivotal clinical trials have broadened the potential of PARPis to the other GU cancers, including urothelial carcinoma and renal cell carcinoma. In this review, we examine the biomarkers for the response to PARPis beyond mutations in BRCA1/2 and discuss the current state and future perspectives of PARPis in GU cancers.
- |||||||||| Journal: Clinical differences among the PARP inhibitors in the first-line treatment of advanced-stage ovarian carcinoma. (Pubmed Central) - Jun 1, 2025
There are treatment outcome differences among the various PARP inhibitors that coincide with a patient's specific homologous recombination deficit (HRD) status; moreover, only single-agent olaparib and olaparib with bevacizumab have conferred a 5-year overall survival benefit...The inclusion of PARP inhibitors has significantly improved survival benefits in advanced-stage ovarian cancer, especially among patients with an identifiable HRD. While there are tolerability differences inherent to the specific PARP inhibitors, not to mention approval distinctions, olaparib is the only PARP inhibitor that has demonstrated consistent overall survival benefits.
- |||||||||| Avastin (bevacizumab) / Roche, Rubraca (rucaparib) / Pharma& Schweiz, Tecentriq (atezolizumab) / Roche
Enrollment closed, Trial completion date: The EndoBARR Trial (Endometrial Bevacizumab, Atezolizumab, Rucaparib) (clinicaltrials.gov) - May 30, 2025 P2, N=30, Active, not recruiting, PARPi are active against PCa with HRR mutations, especially in those with germline or somatic Completed --> Active, not recruiting | Trial completion date: Apr 2023 --> Jan 2026
- |||||||||| Journal, BRCA Biomarker, PARP Biomarker: Identification of novel gene expression patterns and pathways involved in PARP-1 inhibitor resistance. (Pubmed Central) - May 22, 2025
KEGG Pathways "P53 signaling pathway" and "Positive regulation of developmental process(BP)", "endoplasmic reticulum lumen(CC)," and "growth factor binding(MF)", were found to be potentially associated with Olaparib resistance. Five hub genes were identified using PPI networking of which FN1, CCN2, and JUN may play a significant role in the development of Olaparib resistance and could be promising therapeutic and diagnostic biomarkers for dealing with Olaparib resistance in BRCA1/2 mutant breast and ovarian cancer.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz, Lynparza (olaparib) / Merck (MSD), AstraZeneca, Zejula (niraparib) / GSK, J&J
Journal, PARP Biomarker: PARP inhibitors in ovarian cancer: Mechanisms of resistance and implications to therapy. (Pubmed Central) - May 18, 2025 Moreover, we explore other innovative treatment strategies aimed at overcoming specific resistance mechanisms, including the inhibition of ATR, WEE1 and POLQ. We also examine the role of PARPi rechallenge in patients with acquired resistance.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz
Preclinical examination of a 76/77Br-labeled PARP-targeted theranostic in ovarian cancer models (IS_1; 225-226-227 CC) - May 10, 2025 - Abstract #SNMMI2025SNMMI_819; Purpose/Background: [76/77Br]RD1 (fig 1a) is a radiobrominated derivative of the poly-ADP ribose polymerase inhibitor (PARPi) rucaparib... PET/CT scans revealed primarily hepatobiliary clearance of the radiotracer, with the maximal tumor uptake of 4.5% injected activity per gram at 30 minutes post-injection
- |||||||||| Pluvicto (lutetium Lu 177 vipivotide tetraxetan) / Novartis, Xofigo (radium Ra-223 dichloride) / Bayer
Real-world outcomes among patients with metastatic castration-resistant prostate cancer (mCRPC) receiving guideline-recommended therapies after treatment with 177Lu-PSMA-617: A real-world prostate cancer disease observation (PRECISION) data platform analysis. () - Apr 23, 2025 - Abstract #ASCO2025ASCO_5737; Guideline-recommended therapies included abiraterone, enzalutamide, darolutamide, apalutamide, cabazitaxel, docetaxel, pembrolizumab, sipuleucel-T, niraparib, olaparib, talazoparib, rucaparib, and radium-223. In this real-world analysis, the majority of patients who received guideline-recommended therapies after 177Lu-PSMA-617 achieved at least a PSA50 response, suggesting that 177Lu-PSMA-617 treatment does not preclude response to other subsequent therapies.
- |||||||||| Real-world analysis of primary tumor transcriptomes in patients subsequently treated with PARP inhibitors. () - Apr 23, 2025 - Abstract #ASCO2025ASCO_5615;
P=N/A In this real-world study of patients initially presenting with non-metastatic disease who subsequently received PARP inhibitors, transcriptome analysis from the primary tumor revealed the presence of adverse molecular features when disease was still localized. Patients with higher Decipher score, p53 mutation signature and PTEN inactivation tumors at initial testing, could be considered for additional confirmatory genomic or genetic testing and potentially novel trials of PARPi.
- |||||||||| Exploring BET inhibitors as promising agents for solitary fibrous tumor (Villa Ciani) - Apr 3, 2025 - Abstract #SarcomaRC2025SARCOMA_RC_271;
RNA-seq was performed on Illumina NovaSeq X. Results Among seven BETis tested in SFT cells, Mivebresib and BMS-986158 exhibited the lowest IC50 values (INT-SFT: 10.8 nM and 6.23 nM; IEC139: 12.5 nM and 28.8 nM) and, in contrast to other BETis, induced apoptosis at 50 nM (INT-SFT: 32% and 45.9%; IEC139: 27.5% and 34.3%)...Combining BETis with PARPi rucaparib or ATRi berzosertib showed synergistic effects, enhancing apoptotic responses and DNA damage accumulation...In vivo, Mivebresib markedly reduced tumor growth in SFT PDX models, supporting its potential as a targeted therapy. Legal entity responsible for the study The authors.
- |||||||||| Review, Journal, BRCA Biomarker, PARP Biomarker: Update on PARP inhibitors for the treatment of ovarian cancer. (Pubmed Central) - Mar 28, 2025
Currently, several PARPis are FDA-approved in ovarian cancer: (1) olaparib (BRCAm), niraparib (BRCAm and BRCA wild-type [BRCAwt]), and olaparib/bevacizumab (BRCAm and BRCAwt/HRD) as maintenance therapy after platinum in newly diagnosed advanced disease; and (2) olaparib, niraparib, and rucaparib for recurrent BRCAm platinum-sensitive disease. This review discusses PARPi data in the newly diagnosed and recurrent settings, how current FDA approvals have evolved, and PARPi combination data.
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